Evidence map›Paper›PMID 36196170›Full record

ArticleTransactions of the American Clinical and Climatological Association2022

DRUGGING "UNDRUGGABLE" DISEASE-CAUSING PROTEINS: FOCUS ON SIGNAL TRANSDUCER AND ACTIVATOR OF TRANSCRIPTION (STAT) 3.

David J Tweardy

Open access · greenAbstract read
In one paragraph

Article in Transactions of the American Clinical and Climatological Association, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
0.5field-weighted citation impact, top 33% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed, 5 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

1 author.

David J TweardyHOUSTON, TEXAS.

Funding

The University of Texas MD Anderson Cancer Center SPORE in Hepatocellular CarcinomaP50CA217674 · NCI · UNIVERSITY OF TX MD ANDERSON CAN CTR · PI BERETTA, LAURA, KASEB, AHMED · 2019 to 2023
$11.3M
Project 3: Inhibiting Oxidative Phosphorylation in Pancreatic CancerP50CA221707 · NCI · UNIVERSITY OF TX MD ANDERSON CAN CTR · PI KOPETZ, SCOTT, MAITRA, ANIRBAN · 2019 to 2023
$11.0M
Targeting STAT3 for the Treatment of CDK4/6 Inhibitor Resistant Advanced Estrogen Receptor Positive Breast Cancer PatientsR01CA255960 · NCI · UNIVERSITY OF TX MD ANDERSON CAN CTR · PI KHANDAN KEYOMARSI · 2021 to 2026
$2.6M
Targeting Stat1 and Stat3 to Reverse Radioresistance in Head and Neck CancerR21CA191556 · NCI · UNIVERSITY OF TX MD ANDERSON CAN CTR · PI TWEARDY, DAVID JOHN · 2015 to 2016
$363k
MURINE MONOCLONAL ANTIBODIES TO HUMAN RESPIRATORY GLYCOPROTEINZ01CL000021 · CLC · CLINICAL CENTER · PI SHELHAMER, J H · 1987 to 1988
–
CLC NIH HHS 75N90019D00021NCI NIH HHS P50 CA217674NCI NIH HHS P50 CA221707NCI NIH HHS R01 CA255960NCI NIH HHS R21 CA191556ORFDO NIH HHS 75N99019D00021
6 · The paper itself

Abstract

Signal transducer and activator of transcription (STAT) 3 has been assigned to the group of "undruggable" disease-causing proteins, despite its containing a Src-homology (SH) 2 domain, a potential Achilles' heel that has eluded successful targeting by academic and pharmaceutical groups over the past 30 years. Based on mutational and modeling studies, our group developed a unique virtual ligand screening strategy targeting the STAT3 SH2 domain that was coupled to robust biochemical and cellular assays and structure-based medicinal chemistry and led to the identification of TTI-101. TTI-101 represents one of the most advanced, direct, small-molecule inhibitors of an SH2 domain-containing, disease-causing protein in clinical development. TTI-101 is currently being evaluated in a Phase 1 study to determine safety and tolerability in addition to pharmacodynamic effects and efficacy in patients with advanced solid tumors.

Indexed as

NaphtholsSulfonamidesBenzenesulfonamidesHumansLigandsPharmaceutical PreparationsBenzenesulfonamidesC188-9 compoundLigandsNaphtholsPharmaceutical PreparationsSulfonamides

Identifiers

PMID36196170
PMCPMC9480546
OpenAlexW4302275712

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.